Rolapitant

VARUBI

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Pronunciation: roe-LA-pi-tant (va-ROO-bee)

Rolapitant ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Rolapitant ballicule

Rolapitant VARUBI mascot mnemonic cartoon — Visual mnemonic: Rolapitant mascot
**“Ruby Roller paint”**

What it isNK1 receptor antagonist; delayed chemotherapy-induced nausea.

Why this oneA very long half-life covers the whole delayed phase from a single dose.

What limits itIt inhibits CYP2D6 for weeks after one dose, which is easily forgotten. Neutropenia; the IV form was withdrawn for anaphylaxis.

Rolapitant molecular structure (skeletal formula) — Molecular structure: Rolapitant

FDA-approved for

chemo nausea (2015)

FDA label

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FDA dosing	Population	Start	Target	Max
Prevention of delayed nausea/vomiting with emetogenic chemotherapy (with a 5-HT3 antagonist and dexamethasone)	Adults	180 mg single dose	180 mg single dose	180 mg per chemotherapy cycle

Renal Undefined

Hepatic No adjustment for mild-moderate (Child-Pugh A/B); avoid in severe (Child-Pugh C)

Do not administer at intervals shorter than 2 weeks

Instructions

180 mg as a single oral dose within 2 hours before initiation of chemotherapy on Day 1
Give in combination with dexamethasone and a 5-HT3 receptor antagonist
Administer no more frequently than every 2 weeks
Take without regard to meals

Available strengths

tab 90 mg

Contraindications

Concomitant CYP2D6 substrates with a narrow therapeutic index (thioridazine, pimozide) - risk of QT prolongation and Torsades de Pointes
Pediatric patients less than 2 years of age (irreversible impairment of sexual development and fertility in juvenile rats)

Cautions

Moderate CYP2D6 inhibition persists at least 28 days after a single dose - affects thioridazine, pimozide, and other CYP2D6 substrates

Adverse reactions

Neutropenia
Hiccups
Abdominal pain
Decreased appetite
Dizziness
Dyspepsia
Urinary tract infection
Stomatitis
Anemia

Pregnancy Insufficient human data; no adverse developmental effects in animals near human exposures.

Lactation No human data; present in rat milk.

Cost

Rolapitant (VARUBI)

Strength		#/mo	generic $/unit	CostPlus
90 mg	tab	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Rolapitant is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2032 est.

NO BOXED WARNINGS

Principal riskIt inhibits CYP2D6 for weeks after a single dose

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilitySedation, QT prolongation, extrapyramidal symptoms or anticholinergic toxicity vary by receptor target.

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Memory aids: interaction avatars

CYP2D6 inhibitor (moderate)

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